Liquid compositions for soft sustained-release capsules and method for production

Abstract

The invention relates to liquid compositions for production of soft sustained-release capsules. According to the invention, the sustained release of the active agent is obtained by in situ formation of a matrix, more or less consolidated and biodegradable, by physical modification of the capsule contents on coming into contact with digestive juices on the opening thereof. The above leads to a release time of more than one hour for the active agent previously dissolved or dispersed by means of solvents, said release being modulated by addition of appropriate adjuncts. The invention further relates to a method for production of said liquid compositions. The above finds application in the pharmaceutical, cosmetic and dietary fields.

The invention claimed is: 
     
       1. Sustained release viscous liquid compositions for capsules, the compositions comprising:
 (i) at least one liquid matrix ingredient of the inverted latex class, the at least one liquid matrix ingredient creating in situ a biodegradable matrix, more or less compact, due to an instantaneous physical modification of the capsule content immediately after the dissolution of the shell of the capsule; 
 (ii) at least one active ingredient; 
 (iii) at least one solvent for active ingredient solubilization or dispersion; and 
 (iv) at least one ingredient modulating the release of the active ingredient from the matrix formed in situ for more than one hour after dissolution of the shell of the capsule. 
 
     
     
       2. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the instantaneous physical modification of the capsule content is obtained from the inverted latexes. 
     
     
       3. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the instantaneous physical modification of the capsule content is a jellification or reticulation of the liquid matrix ingredient under digestive secretion contact. 
     
     
       4. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the instantaneous physical modification of the capsule content occurs between 1 second and 10 minutes after opening of the capsule. 
     
     
       5. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the inverted latexes are derivatives of acrylic acid or of acrylamide polymers. 
     
     
       6. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the at least one liquid matrix ingredient represents 0.1 to 100% of the total mass of the ingredients. 
     
     
       7. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the viscosity of the liquid composition is between 50 millipascals and 500,000 millipascals. 
     
     
       8. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the active ingredients belong to therapeutic classes. 
     
     
       9. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the active ingredient is in the liquid state or dispersed in the solvent. 
     
     
       10. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the active ingredient is dissolved or dispersed in oils or organic solvents having a lipophilic, hydrophilic or hydrolipophilic nature. 
     
     
       11. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the active ingredient is in the solid state and dispersed in uncoated powder form, coated powder form, or an absorbent. 
     
     
       12. Sustained release viscous liquid compositions for capsules according to  claim 11 , wherein the active ingredient in the solid state has a granulometry between 1 μm to 100 μm. 
     
     
       13. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the ingredient modulating the release kinetics of the active ingredient is selected from the group consisting of hydrophilic additives, plasticizers, tensioactives, dissolution accelerators class and buffer systems. 
     
     
       14. Sustained release viscous liquid compositions for capsules according to  claim 13 , wherein the ingredient modulating the release kinetics of the active ingredient is a hydrophilic additive is selected from the group consisting of cellulose and cellulose derivatives, starches and their derivatives, polysaccharides, and polymers of vinylpyrrolidone. 
     
     
       15. Sustained release viscous liquid compositions for capsules according to  claim 13 , wherein the ingredient modulating the release kinetics of the active ingredient is a hydrophilic additive having a concentration between 0% and 80% by weight with respect to the total mass of the ingredients. 
     
     
       16. Sustained release viscous liquid compositions for capsules according to  claim 13 , wherein the ingredient modulating the release kinetics of the active ingredient is a hydrophilic additive having a granulometry between 1 μm and 1000 μm. 
     
     
       17. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the release of the active ingredient from such matrices varies from one hour to twenty-four hours. 
     
     
       18. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the composition is conditioned in a hard or a soft capsule. 
     
     
       19. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the composition of the capsule shell is selected from the group consisting of gelatin, starches, hydroxypropylmethylcellulose, carrageenan and polyvinylic alcohol polymers. 
     
     
       20. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the concentration of solid material in the liquid matrix ingredients is between 0.1% and 90% by weight to the volume of the liquid matrix ingredients. 
     
     
       21. Sustained release viscous liquid compositions for capsules according to  claim 1 , wherein the invert latexes are liquid polymers coming from the polymerization of a liquid medium containing an acrylate or acrylamide monomer, an oily phase, an aqueous phase, a tensioactive of the type water-in-oil, a tensioactive of the type oil-in-water, and a complexing agent.